Azelastine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : Ophthalmic Seasonal and perennial allergic conjunctivitis As 0.05% solution: Instill 1 drop into affected eye(s) bid, may increase to 4 times/day. Max duration: 6 weeks. Nasal Allergic rhinitis As spray: 140 mcg in each nostril bid.
Dosage Details
Nasal
Allergic rhinitis
Adult: As spray: 140 mcg into each nostril bid.
Child: ≥6 years Same as adult dose.

Ophthalmic
Seasonal allergic conjunctivitis
Adult: As 0.05% solution: Instill 1 drop into affected eye(s) bid. For severe cases, increase to 4 times daily. Max duration: 6 weeks.
Child: ≥4 years Same as adult dose.

Ophthalmic
Allergic conjunctivitis, perennial
Adult: As 0.05% solution: Instill 1 drop into affected eye(s) bid. For severe cases, increase to 4 times daily. Max duration: 6 weeks.
Child: ≥12 years Same as adult dose.
Special Precautions
Pregnancy and lactation.
Adverse Reactions
Significant: Irritation of nasal mucosa (e.g. stinging, itching, sneezing, epistaxis) and eyes (e.g. burning, pain), conjunctivitis.
Gastrointestinal disorders: Dry mouth. Rarely, nausea.
General disorders and administration site conditions: Fatigue.
Nervous system disorders: Headache, bitter taste.
Psychiatric disorders: Somnolence.
Inhalation/Respiratory/Nasal/Ophth: C
Patient Counseling Information
Avoid contact with soft contact lenses. This drug may cause somnolence and eye irritation, if affected, do not drive or operate machinery.
Drug Interactions
Reduced CNS function and alertness with CNS depressants.
Food Interaction
Reduced CNS function and alertness with alcohol.
Action
Description: Azelastine, a phthalazinone derivative, selectively blocks H1-receptors on effector cells, inhibiting the release of histamine involved in allergic response. Additionally, it inhibits the accumulation of other inflammatory mediators like leukotriene, platelet activation factor (PAF), serotonin, and eosinophil.
Onset: 15-30 minutes (nasal).
Duration: 8 hours (ophthalmic); 12 hours (nasal).
Pharmacokinetics:
Absorption: Ocular absorption is low. Nasal: Bioavailability: Approx 40%. Time to peak plasma concentration: 4 hours.
Distribution: Plasma protein binding: Approx 88%.
Metabolism: Metabolised in the liver by CYP isoenzyme into the major metabolite, N-desmethylazelastine.
Excretion: Mainly via faeces (approx 75%, <10% as unchanged drug) and urine. Elimination half-life: 22-25 hours (nasal).
Chemical Structure

Chemical Structure Image
Azelastine

Source: National Center for Biotechnology Information. PubChem Database. Azelastine, CID=2267, https://pubchem.ncbi.nlm.nih.gov/compound/Azelastine (accessed on Jan. 21, 2020)

Storage
Ophthalmic solution: Store between 2-25°C. Nasal spray: Store between 20-25°C. Protect from freezing.
ATC Classification
R01AC03 - azelastine ; Belongs to the class of topical antiallergic preparations, excluding corticosteroids. Used as antiallergic agents.
S01GX07 - azelastine ; Belongs to the class of other ophthalmologic antiallergics.
References
Anon. Azelastine (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/10/2016.

Anon. Azelastine (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/10/2016.

Anon. Azelastine Hydrochloride (EENT). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 20/10/2016.

Azelastine HCl Nasal Spray (Perrigo New York Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/10/2016.

Azelastine Hydrochloride Solution/Drops (Wallace Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 20/10/2016.

Buckingham R (ed). Azelastine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/10/2016.

Joint Formulary Committee. Azelastine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/10/2016.

Disclaimer: This information is independently developed by MIMS based on Azelastine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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